Compounds > amg 221
Page last updated: 2024-08-04 06:00:51

amg 221

Description

AMG 221: structure in first source [MeSH]

Cross-References

ID SourceID
PubMed CID135565424
CHEMBL ID1085107
SCHEMBL ID10284762
SCHEMBL ID23798787
MeSH IDM0537202

Synonyms (20)

Synonym
CHEMBL1085107 ,
amg-221
bdbm50319665
(s)-2-((1s,2s,4r)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5h)-one
4(5h)-thiazolone, 2-((1s,2s,4r)-bicyclo(2.2.1)hept-2-ylamino)-5-methyl-5-(1-methylethyl)-, (5s)-
2t929w7ag8 ,
1095565-81-3
unii-2t929w7ag8
amg 221
948044-21-1
bvt-83370
SCHEMBL10284762
Q27255579
(5s)-2-[[(1s,2s,4r)-2-bicyclo[2.2.1]heptanyl]imino]-5-methyl-5-propan-2-yl-1,3-thiazolidin-4-one
(5s)-2-[[(1s,2s,4r)-2-bicyclo[2.2.1]heptanyl]amino]-5-methyl-5-propan-2-yl-1,3-thiazol-4-one
cid 25207668
HY-10555
CS-0002637
SCHEMBL23798787
AKOS040747810

Protein Targets (9)

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)
Glucocorticoid receptorHomo sapiens (human)IC5010.0000AID483785
Cytochrome P450 1A2Homo sapiens (human)IC5015.0000AID483804
Cytochrome P450 3A4Homo sapiens (human)IC5015.0000AID483802
Cytochrome P450 2D6Homo sapiens (human)IC5015.0000AID483803
Cytochrome P450 2C9 Homo sapiens (human)IC5015.0000AID483805
Corticosteroid 11-beta-dehydrogenase isozyme 1Homo sapiens (human)IC503.3401AID483782; AID483784; AID657806
Corticosteroid 11-beta-dehydrogenase isozyme 1Homo sapiens (human)Ki0.0128AID483781; AID657805
Cytochrome P450 2C19Homo sapiens (human)IC5015.0000AID483806
Corticosteroid 11-beta-dehydrogenase isozyme 1Mus musculus (house mouse)Ki0.0708AID657807
Corticosteroid 11-beta-dehydrogenase isozyme 2Homo sapiens (human)IC5010.0000AID483783

Bioassays (61)

Assay IDTitleYearJournalArticle
AID483790Clearance in Sprague-Dawley rat at 5 mg/kg, iv or 30 mg/kg, po2010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
ISSN: 1520-4804		Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221).
AID483800Terminal half life in cynomolgus monkey at 5 mg/kg, iv or 30 mg/kg, po2010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
ISSN: 1520-4804		Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221).
AID657810Terminal half life in Sprague-Dawley rat at 2 mg/kg, iv and 10 mg/kg, po2011ACS medicinal chemistry letters, Nov-10, Volume: 2, Issue:11
ISSN: 1948-5875		Synthesis and Evaluation of the Metabolites of AMG 221, a Clinical Candidate for the Treatment of Type 2 Diabetes.
AID657844Plasma protein binding in po dosed mouse after 4 hrs2011ACS medicinal chemistry letters, Nov-10, Volume: 2, Issue:11
ISSN: 1948-5875		Synthesis and Evaluation of the Metabolites of AMG 221, a Clinical Candidate for the Treatment of Type 2 Diabetes.
AID1151435Inhibition of adipose tissue-derived 11beta-HSD1 (unknown origin) assessed as concentration required for maximal inhibition2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
ISSN: 1520-4804		Medicinal chemistry of inhibitors of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1).
AID483802Inhibition of CYP3A42010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
ISSN: 1520-4804		Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221).
AID483804Inhibition of CYP1A22010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
ISSN: 1520-4804		Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221).
AID657808Clearance in Sprague-Dawley rat at 2 mg/kg, iv and 10 mg/kg, po2011ACS medicinal chemistry letters, Nov-10, Volume: 2, Issue:11
ISSN: 1948-5875		Synthesis and Evaluation of the Metabolites of AMG 221, a Clinical Candidate for the Treatment of Type 2 Diabetes.
AID483806Inhibition of CYP2C192010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
ISSN: 1520-4804		Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221).
AID483808Ex vivo inhibition of 11beta-HSD1 in high fat diet-fed C57BL/6 mouse inguinal fat at 5 mg/kg, po measured at 4 hrs by ELISA2010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
ISSN: 1520-4804		Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221).
AID483792Terminal half life in Sprague-Dawley rat at 5 mg/kg, iv or 30 mg/kg, po2010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
ISSN: 1520-4804		Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221).
AID657826Ratio of drug level in adipose tissue fat to plasma of mouse at 50 mg/kg, po2011ACS medicinal chemistry letters, Nov-10, Volume: 2, Issue:11
ISSN: 1948-5875		Synthesis and Evaluation of the Metabolites of AMG 221, a Clinical Candidate for the Treatment of Type 2 Diabetes.
AID483807Metabolic stability in liver microsomes2010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
ISSN: 1520-4804		Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221).
AID483788Terminal half life in CD1 mouse at 5 mg/kg, iv or 30 mg/kg, po2010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
ISSN: 1520-4804		Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221).
AID657812Oral bioavailability in Sprague-Dawley rat at 10 mg/kg2011ACS medicinal chemistry letters, Nov-10, Volume: 2, Issue:11
ISSN: 1948-5875		Synthesis and Evaluation of the Metabolites of AMG 221, a Clinical Candidate for the Treatment of Type 2 Diabetes.
AID1151434Inhibition of adipose tissue-derived 11beta-HSD1 (unknown origin)2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
ISSN: 1520-4804		Medicinal chemistry of inhibitors of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1).
AID483787Volume of distribution at steady state in CD1 mouse at 5 mg/kg, iv or 30 mg/kg, po2010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
ISSN: 1520-4804		Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221).
AID1071798Inhibition of 11beta-HSD1 in mouse liver microsomes using cortisone as substrate after 2 hrs by HTRF assay2014Bioorganic & medicinal chemistry letters, Mar-01, Volume: 24, Issue:5
ISSN: 1464-3405		3-Amino-N-adamantyl-3-methylbutanamide derivatives as 11β-hydroxysteroid dehydrogenase 1 inhibitor.
AID657805Inhibition of human 11beta-HSD1 expressed in Escherichia coli using [3H]cortisone as substrate by scintillation proximity assay2011ACS medicinal chemistry letters, Nov-10, Volume: 2, Issue:11
ISSN: 1948-5875		Synthesis and Evaluation of the Metabolites of AMG 221, a Clinical Candidate for the Treatment of Type 2 Diabetes.
AID483812Ex vivo inhibition of 11beta-HSD1 in high fat diet-fed C57BL/6 mouse inguinal fat at 15 mg/kg, po measured at 8 hrs by ELISA2010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
ISSN: 1520-4804		Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221).
AID657815Half life in CD1 mouse at 2 mg/kg, iv and 10 mg/kg, po2011ACS medicinal chemistry letters, Nov-10, Volume: 2, Issue:11
ISSN: 1948-5875		Synthesis and Evaluation of the Metabolites of AMG 221, a Clinical Candidate for the Treatment of Type 2 Diabetes.
AID483821Antiobesity activity in diet-induced obese mouse assessed as decrease in body weight at 5 mg/kg administered QD via high fat-diet for 13 days measured after day 132010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
ISSN: 1520-4804		Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221).
AID1218573Oral bioavailability in rat2012Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
ISSN: 1521-009X		Regiospecific and stereospecific triangulation of the structures of metabolites formed by sequential metabolism at multiple prochiral centers.
AID657813Clearance in CD1 mouse at 2 mg/kg, iv and 10 mg/kg, po2011ACS medicinal chemistry letters, Nov-10, Volume: 2, Issue:11
ISSN: 1948-5875		Synthesis and Evaluation of the Metabolites of AMG 221, a Clinical Candidate for the Treatment of Type 2 Diabetes.
AID483803Inhibition of CYP2D62010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
ISSN: 1520-4804		Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221).
AID1218574Volume of distribution at steady state in rat2012Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
ISSN: 1521-009X		Regiospecific and stereospecific triangulation of the structures of metabolites formed by sequential metabolism at multiple prochiral centers.
AID483801Bioavailability in cynomolgus monkey at 5 mg/kg, iv or 30 mg/kg, po2010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
ISSN: 1520-4804		Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221).
AID483794Clearance in Beagle dog at 5 mg/kg, iv or 30 mg/kg, po2010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
ISSN: 1520-4804		Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221).
AID483797Bioavailability in Beagle dog at 5 mg/kg, iv or 30 mg/kg, po2010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
ISSN: 1520-4804		Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221).
AID483805Inhibition of CYP2C92010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
ISSN: 1520-4804		Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221).
AID483789Bioavailability in CD1 mouse at 5 mg/kg, iv or 30 mg/kg, po2010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
ISSN: 1520-4804		Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221).
AID483799Volume of distribution at steady state in cynomolgus monkey at 5 mg/kg, iv or 30 mg/kg, po2010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
ISSN: 1520-4804		Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221).
AID483795Volume of distribution at steady state in Beagle dog at 5 mg/kg, iv or 30 mg/kg, po2010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
ISSN: 1520-4804		Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221).
AID1218572Plasma protein binding in rat2012Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
ISSN: 1521-009X		Regiospecific and stereospecific triangulation of the structures of metabolites formed by sequential metabolism at multiple prochiral centers.
AID657806Inhibition of human 11beta-HSD1 expressed in CHO cells2011ACS medicinal chemistry letters, Nov-10, Volume: 2, Issue:11
ISSN: 1948-5875		Synthesis and Evaluation of the Metabolites of AMG 221, a Clinical Candidate for the Treatment of Type 2 Diabetes.
AID1218571Plasma protein binding in human2012Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
ISSN: 1521-009X		Regiospecific and stereospecific triangulation of the structures of metabolites formed by sequential metabolism at multiple prochiral centers.
AID657843Free plasma concentration in po dosed mouse after 4 hrs2011ACS medicinal chemistry letters, Nov-10, Volume: 2, Issue:11
ISSN: 1948-5875		Synthesis and Evaluation of the Metabolites of AMG 221, a Clinical Candidate for the Treatment of Type 2 Diabetes.
AID483815Antidiabetic activity in diet-induced obese mouse assessed as decrease in plasma insulin level at 25 to 50 mg/kg, po administered via gavage BID for 13 days measured after day 13 by glucose tolerance test2010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
ISSN: 1520-4804		Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221).
AID483818Antidiabetic activity in diet-induced obese mouse assessed as mild improvement of glucose tolerance at 25 to 50 mg/kg, ip BID for 13 days measured on day 14 after 12 hrs of fasting by glucose tolerance test2010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
ISSN: 1520-4804		Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221).
AID483782Displacement of [3H]-cortisone human 17beta-HSD1 expressed in HEK293 cells after 30 mins by scintillation proximity assay2010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
ISSN: 1520-4804		Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221).
AID657816Oral bioavailability in CD1 mouse at 10 mg/kg2011ACS medicinal chemistry letters, Nov-10, Volume: 2, Issue:11
ISSN: 1948-5875		Synthesis and Evaluation of the Metabolites of AMG 221, a Clinical Candidate for the Treatment of Type 2 Diabetes.
AID483785Inhibition of glucocorticoid receptor2010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
ISSN: 1520-4804		Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221).
AID483813Ex vivo inhibition of 11beta-HSD1 in high fat diet-fed C57BL/6 mouse inguinal fat at 50 mg/kg, po measured at 8 hrs by ELISA2010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
ISSN: 1520-4804		Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221).
AID483784Inhibition of 11beta-HSD12010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
ISSN: 1520-4804		Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221).
AID483810Ex vivo inhibition of 11beta-HSD1 in high fat diet-fed C57BL/6 mouse inguinal fat at 50 mg/kg, po measured at 4 hrs by ELISA2010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
ISSN: 1520-4804		Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221).
AID657807Inhibition of mouse 11beta-HSD1 expressed in Escherichia coli using [3H]cortisone as substrate by scintillation proximity assay2011ACS medicinal chemistry letters, Nov-10, Volume: 2, Issue:11
ISSN: 1948-5875		Synthesis and Evaluation of the Metabolites of AMG 221, a Clinical Candidate for the Treatment of Type 2 Diabetes.
AID483820Antiobesity activity in po dosed diet-induced obese mouse assessed as decrease in body weight administered via gavage BID for 13 days measured after day 132010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
ISSN: 1520-4804		Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221).
AID483793Bioavailability in Sprague-Dawley rat at 5 mg/kg, iv or 30 mg/kg, po2010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
ISSN: 1520-4804		Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221).
AID483781Displacement of [3H]-cortisone human 17beta-HSD1 expressed in Escherichia coli after 30 mins by scintillation proximity assay2010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
ISSN: 1520-4804		Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221).
AID483798Clearance in cynomolgus monkey at 5 mg/kg, iv or 30 mg/kg, po2010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
ISSN: 1520-4804		Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221).
AID657809Volume of distribution at steady state in Sprague-Dawley rat at 2 mg/kg, iv and 10 mg/kg, po2011ACS medicinal chemistry letters, Nov-10, Volume: 2, Issue:11
ISSN: 1948-5875		Synthesis and Evaluation of the Metabolites of AMG 221, a Clinical Candidate for the Treatment of Type 2 Diabetes.
AID483783Inhibition of 11beta-HSD22010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
ISSN: 1520-4804		Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221).
AID1218575Clearance in iv dosed rat2012Drug metabolism and disposition: the biological fate of chemicals, May, Volume: 40, Issue:5
ISSN: 1521-009X		Regiospecific and stereospecific triangulation of the structures of metabolites formed by sequential metabolism at multiple prochiral centers.
AID483791Volume of distribution at steady state in Sprague-Dawley rat at 5 mg/kg, iv or 30 mg/kg, po2010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
ISSN: 1520-4804		Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221).
AID657814Volume of distribution at steady state in CD1 mouse at 2 mg/kg, iv and 10 mg/kg, po2011ACS medicinal chemistry letters, Nov-10, Volume: 2, Issue:11
ISSN: 1948-5875		Synthesis and Evaluation of the Metabolites of AMG 221, a Clinical Candidate for the Treatment of Type 2 Diabetes.
AID483811Ex vivo inhibition of 11beta-HSD1 in high fat diet-fed C57BL/6 mouse inguinal fat at 5 mg/kg, po measured at 8 hrs by ELISA2010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
ISSN: 1520-4804		Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221).
AID483814Antidiabetic activity in diet-induced obese mouse assessed as decrease in fed blood glucose level at 25 to 50 mg/kg, po administered via gavage BID for 13 days measured after day 13 by glucose tolerance test2010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
ISSN: 1520-4804		Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221).
AID483786Clearance in CD1 mouse at 5 mg/kg, iv or 30 mg/kg, po2010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
ISSN: 1520-4804		Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221).
AID483809Ex vivo inhibition of 11beta-HSD1 in high fat diet-fed C57BL/6 mouse inguinal fat at 15 mg/kg, po measured at 4 hrs by ELISA2010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
ISSN: 1520-4804		Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221).
AID1071799Inhibition of 11beta-HSD1 in human liver microsomes using cortisone as substrate after 2 hrs by HTRF assay2014Bioorganic & medicinal chemistry letters, Mar-01, Volume: 24, Issue:5
ISSN: 1464-3405		3-Amino-N-adamantyl-3-methylbutanamide derivatives as 11β-hydroxysteroid dehydrogenase 1 inhibitor.
AID483796Terminal half life in Beagle dog at 5 mg/kg, iv or 30 mg/kg, po2010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
ISSN: 1520-4804		Discovery of a potent, orally active 11beta-hydroxysteroid dehydrogenase type 1 inhibitor for clinical study: identification of (S)-2-((1S,2S,4R)-bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221).

Research

Studies (9)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's1 (11.11)29.6817
2010's8 (88.89)24.3611
2020's0 (0.00)2.80

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials1 (11.11%)5.53%
Reviews1 (11.11%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other7 (77.78%)84.16%
SubstanceStudiesClassesRolesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
rosiglitazone
1
aminopyridine;
thiazolidinediones		EC 6.2.1.3 (long-chain-fatty-acid--CoA ligase) inhibitor;
ferroptosis inhibitor;
insulin-sensitizing drug		2010201014.0low000100
3-(1-adamantyl)-6,7,8,9-tetrahydro-5h-(1,2,4)triazolo(4,3-a)azepine
1
2014201410.0high000010
bvt2733
1
2014201410.0high000010
mk-0916
1
2014201410.0high000010
pf 877423
1
2014201410.0high000010
pf 915275
1
2014201410.0medium000010
SubstanceStudiesClassesRolesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
chlorine
1
halide anion;
monoatomic chlorine		cofactor;
Escherichia coli metabolite;
human metabolite		2009200915.0low000100
thiazoles
6
1,3-thiazoles;
mancude organic heteromonocyclic parent;
monocyclic heteroarene		2009201412.5high100240
2-aminothiazoline
1
1,3-thiazoles;
primary amino compound		2009200915.0medium000100
ConditionIndicatedStudiesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
Acute Confusional Senile Dementia0
1
2014201410.0medium000010
Alzheimer Disease0
1
2014201410.0medium000010
Cardiometabolic Syndrome0
1
2014201410.0medium000010
Cardiovascular Diseases0
1
2014201410.0medium000010
Glaucoma0
1
2014201410.0medium000010
Metabolic Syndrome0
1
2014201410.0medium000010
Obesity0
1
2011201113.0medium100010

Safety/Toxicity (1)

ArticleYear
Activity-based exposure comparisons among humans and nonclinical safety testing species in an extensively metabolized drug candidate.
Xenobiotica; the fate of foreign compounds in biological systems, , Volume: 43, Issue:7		2013

Pharmacokinetics (1)

ArticleYear
Population pharmacokinetic/pharmacodynamic model of subcutaneous adipose 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) activity after oral administration of AMG 221, a selective 11β-HSD1 inhibitor.
Journal of clinical pharmacology, , Volume: 51, Issue:6		2011

Bioavailability (2)

ArticleYear
Synthesis and Evaluation of the Metabolites of AMG 221, a Clinical Candidate for the Treatment of Type 2 Diabetes.
ACS medicinal chemistry letters, , Nov-10, Volume: 2, Issue:11		2011
Intestinal and hepatic first-pass extraction of the 11β-HSD1 inhibitor AMG 221 in rats with chronic vascular catheters.
Xenobiotica; the fate of foreign compounds in biological systems, , Volume: 44, Issue:3		2014

Dosage (2)

ArticleYear
Activity-based exposure comparisons among humans and nonclinical safety testing species in an extensively metabolized drug candidate.
Xenobiotica; the fate of foreign compounds in biological systems, , Volume: 43, Issue:7		2013
Regiospecific and stereospecific triangulation of the structures of metabolites formed by sequential metabolism at multiple prochiral centers.
Drug metabolism and disposition: the biological fate of chemicals, , Volume: 40, Issue:5		2012